CAS NO: | 357-70-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with anIC50of 500 nM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Galanthamine inhibits AChE and BChE with IC50of 0.5 and 8.5 μM[1]. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes[2]. | ||||||||||||||||
体内研究 (In Vivo) | Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 287.35 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C17H21NO3 | ||||||||||||||||
CAS 号 | 357-70-0 | ||||||||||||||||
中文名称 | 加兰他敏;加兰他明;尼瓦林;强肌;雪花胺;雪花莲胺 | ||||||||||||||||
结构分类 |
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来源 |
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 59 mg/mL(205.32 mM) 1M HCl : 50 mg/mL(174.00 mM;ultrasonic and adjust pH to 1 with HCl) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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